Astex Therapeutics Limited

Novartis Ag

Otsuka Pharmaceutical Company, Limited

Taiho Pharmaceutical Company Limited

Cancer Research Technology Limited

Steven Douglas Hiscock

Steven Howard

Gianni Chessari

Andrew James Woodhead

Christopher Charles Frederick Hamlett

Jeffrey David St Denis

Miles Stuart Congreve

Christopher Norbert Johnson

Michael Luzzio

Ildiko Maria Buck

Alison Jo-Anne Woolford

Bharat Lagu

Lawrence Blas Perez

Charlotte Mary Griffiths-Jones

Gilbert Besong

Maria Grazia Carr

Fan Yang

Christopher Thomas Brain

Christine Hiu-Tung Chen

James Edward Harvey Day

David Norton

Kim Louise Hirst

Jeremy Peter Scott

Neil Thomas Thompson

Yaping Wang

Young Shin Cho

James Daniel Osborne

David Cousin

John William Giraldes

Rhian Sara Holvey

Sunkyu Kim

Claudio Dagostin

Brian Christopher Bishop

Marc O'Reilly

Hendrika Maria Gerarda Willems

Nicholas John Palmer

Yipin Lu

Darren James Dixon

Paul Mortenson

Alessia Millemaggi

John Walter Liebeschuetz

Hideto Fujiwara

Peter Richard Mullens

Aaron Michael Dumas

David Parry-Jones

Meenakshi Sundaram Shanmugham

Matthew James Gaunt

Jonas Calleja Priede

Alan Richard Burns

David Geoffrey Twigg

Susanne Maria Saalau-Bethell

Michael Joseph Luzzio

Paul Neil Mortenson

John Grialdes

The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.

Isoindolinone inhibitors of the MDM2-P53 interaction and process for making them

The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Pharmaceutical compounds

The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): or a salt, N-oxide, tautomer or stereoisomer thereof, wherein A is CH or N; E is CH or N;

The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof;wherein Q is CH or N; X is N, N&#x2014;Oor CR; Y is N, N&#x2014;Oor CR; Rand Rare independently selected from hydrogen and various substituents as defined in the claims; or Rand Rtogether with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; Ris selected from hydrogen and various substituents; and Ris selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

Imidazole derivatives and their use as modulators of cyclin dependent kinases

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Royston, United Kingdom

Steven Douglas Hiscock